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Lisinopril is a medication belonging to the drug class of angiotensin-converting enzyme (ACE) inhibitors and is used to treat hypertension (high blood pressure), heart failure, and heart attacks. It is available as a generic medication. It is available in combination with amlodipine (as lisinopril/amlodipine) and in combination with hydrochlorothiazide (as lisinopril/hydrochlorothiazide).
Medical uses
Lisinopril is typically used for the treatment of high blood pressure, congestive heart failure, and diabetic nephropathy and after acute myocardial infarction (heart attack).
Adverse effects
Common side effects include headache, dizziness, feeling tired, cough, nausea, and rash. People may present to dental care suspicious of an infected tooth, but the swelling around the mouth may be due to lisinopril-induced angioedema, prompting emergency and medical referral. Unlike other ACE inhibitors, it is not a prodrug, is not metabolized by the liver, and is excreted unchanged in the urine. The inhibition of the RAAS system causes an overall decrease in blood pressure. Declining serum concentrations exhibit a prolonged terminal phase, which does not contribute to drug accumulation. This terminal phase probably represents saturable binding to ACE and is not proportional to dose. Lisinopril does not undergo metabolism and the absorbed drug is excreted unchanged entirely in the urine. Based on urinary recovery, the mean extent of absorption of lisinopril is approximately 25% (reduced to 16% in people with New York Heart Association Functional Classification (NYHA) Class II–IV heart failure), with large interpatient variability (6 to 60%) at all doses tested (5 to 80 mg). Lisinopril absorption is not affected by the presence of food in the gastrointestinal tract.
Studies in rats indicate that lisinopril crosses the blood-brain barrier poorly. Multiple doses of lisinopril in rats result in little or no accumulation in brain tissue.
Distribution
Lisinopril does not bind to proteins in the blood. The full duration of action is between 24 and 30 hours. less soluble in methanol, and virtually insoluble in ethanol. Enalapril is a derivative, designed by scientists at Merck to overcome the rash and bad taste caused by captopril.
Enalapril is actually a prodrug; the active metabolite is enalaprilat.
The di-acid metabolite of enalapril, enalaprilat, and its lysine analogue lisinopril are potent inhibitors of angiotensin-converting enzyme (ACE); they do not contain sulphydryl groups. Both drugs can be assayed by high-pressure liquid chromatography and by radioimmunoassay and plasma ACE inhibition remains stable under normal storage conditions. It is therefore possible to study their pharmacokinetics as well as their pharmacodynamic effects in humans. Enalaprilat and lisinopril as well as ACE activity have been measured in blood taken during the course of two studies of the effects of these drugs on blood pressure and autonomic responsiveness.
Lisinopril is a synthetic peptide derivative of captopril. The drug became a blockbuster for AstraZeneca (formed in 1998), with annual sales in 1999 of $1.2B. Since then, lisinopril has been available under many brand names worldwide; it is also available in combination drugs with diuretic hydrochlorothiazide (as lisinopril/hydrochlorothiazide), and with calcium channel blocker amlodipine (as lisinopril/amlodipine).
Society and culture
Legal status
In July 2016, an oral solution formulation of lisinopril was approved for use in the United States.